24131-30-4Relevant articles and documents
Synthesis of (E)-2,3′,4,5′-tetramethoxy[2-11C] stilbene
Schweiger, Lutz,Craib, Stuart,Welch, Andrew,Smith, Tim A. D.
, p. 1206 - 1210 (2007)
In this paper, we describe the radiosynthesis of the compound (E)-2,3′,4,5′-tetramethoxy[2-11C]stilbene, a potential, universal tumour positron emission tomography imaging agent. The production of (E)-2,3′,4,5′-tetramethoxy[2-11C]sti
FGFR4 INHIBITORS
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Page/Page column 47, (2016/10/31)
Methods, compounds, pharmaceutical compositions, and methods of preparing medicaments for treating hepatocellular carcinoma having an altered FGFR4 and/or FGF19 status.
Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators
Nomura, Sayaka,Endo-Umeda, Kaori,Aoyama, Atsushi,Makishima, Makoto,Hashimoto, Yuichi,Ishikawa, Minoru
supporting information, p. 902 - 907 (2015/08/24)
Anti-inflammatory effects of liver X receptor (LXR) ligands are thought to be largely due to LXR-mediated transrepression, whereas side effects are caused by activation of LXR-responsive gene expression (transactivation). Therefore, selective LXR modulators that preferentially exhibit transrepression activity should exhibit anti-inflammatory properties with fewer side effects. Here, we synthesized a series of styrylphenylphthalimide analogues and evaluated their structure-activity relationships focusing on LXRs-transactivating-agonistic/antagonistic activities and transrepressional activity. Among the compounds examined, 17l showed potent LXR-transrepressional activity with high selectivity over transactivating activity and did not show characteristic side effects of LXR-transactivating agonists in cells. This representative compound, 17l, was confirmed to have LXR-dependent transrepressional activity and to bind directly to LXRβ. Compound 17l should be useful not only as a chemical tool for studying the biological functions of LXRs transrepression but also as a candidate for a safer agent to treat inflammatory diseases.